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NMS-P715
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NMS-P715图片
CAS NO:1202055-32-0
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
NMS-P715 是一种选择性的,ATP 竞争性的MPS1抑制剂,IC50值为 182 nM。
生物活性

NMS-P715 is a selective, ATP-competitive inhibitor ofMPS1, with anIC50of 182 nM.

IC50& Target[1]

Mps1

182 nM (IC50)

CK2

5.7 μM (IC50)

MELK

6.01 μM (IC50)

NEK6

6.02 μM (IC50)

体外研究
(In Vitro)

NMS-P715 is a selective inhibitor of MPS1, with an IC50of 182 nM. NMS-P715 is highly specific for MPS1, with no other kinases inhibited below an IC50value of 5 μM and only 3 kinases inhibited below 10 μM (CK2, MELK, and NEK6). NMS-P715 promotes massive spindle assembly checkpoint (SAC) override with an EC50of 65 nM. NMS-P715 (1 μM) causes mitotic acceleration in U2OS cells overexpressing YFP-α-tubulin, induces aneuploidy and inhibits the proliferation of HCT116 cells. NMS-P715 (0.5, 1 μM) affects mitotic checkpoint complex (MCC) stability and cdc20 ubiquitylation[1]. NMS-P715 (1 μM) exhibits bypass of the spindle assembly checkpoint and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. NMS-P715 (0-25 μM) also selectively inhibits growth of PDAC cells[2].

体内研究
(In Vivo)

NMS-P715 (10 mg/kg) exhibits an oral bioavailability of 37% and good pharmacokinetic properties in nude mice bearing subcutaneous implanted human tumor cell xenografts. NMS-P715 (90 mg/kg, p.o.) is well tolerated and cuases no signs of body weight loss or other overt toxicities in an A2780 ovary carcinoma xenograft model. NMS-P715 (100 mg/kg, p.o.) inhibits the tumor growth by appr 43% in the A375 melanoma xenograft model[1].

分子量

676.73

性状

Solid

Formula

C35H39F3N8O3

CAS 号

1202055-32-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 2 mg/mL(2.96 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.4777 mL7.3885 mL14.7769 mL
5 mM---------
10 mM---------
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 0.5% CMC/saline water

    Solubility: 3.33 mg/mL (4.92 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在本网站选购。